Approaches to enhance solubility and dissolution of poorly water soluble drug: Satranidazole

Chilukala, Swathi; Aparna, C.; Shastri, Nalini; M., Sadanandam
November 2011
Journal of Pharmacy Research;Nov2011, Vol. 4 Issue 11, p4135
Academic Journal
Satranidazole is poorly soluble in water. Its gastrointestinal absorption is limited by its solubility and dissolution rate. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. Hence an attempt was made to enhance the solubility and dissolution rate. Various techniques were used to enhance the solubility and dissolution rate. They are cosolvency, hydrotropy, solid dispersion and surface solid dispersion. Various solvents and cosolvents in combinations were used for solubility enhancement of Satranidazole. Hydrotropes like sodium benzoate and sodium salicylate in various concentrations were used for solubility enhancement of Satranidazole. Both the techniques have shown enhanced solubility, but maximum enhancement in solubility was found to be in 2M sodium salicylate by using hydrotropy. Solid dispersions were prepared by fusion method and solvent evaporation method using various carriers, like PEG 4000, PEG 6000, Polaxomer-407, PVP-K30 and HPMC. Surface solid dispersions were prepared by solvent deposition technique using crospovidone, croscarmellose, sodium starch glycolate, pregelatinized starch, and avicel pH 101. The formulations were characterized by powder X-ray diffractometry, differential scanning calorimetry and scanning electron microscopy. Wettability, hygroscopicity, solubility and in- vitro dissolution studies were performed. The dissolution rate of the drug on SSG based surface solid dispersion was significantly higher than other excipients based preparations. The dissolution rate of the drug on PVP and polaxomer based solid dispersions were significantly higher than other excipients based preparations. All the solid dispersions and surface solid dispersions showed dissolution improvement vis-à-vis pure drug to varying degrees, with PVP, PXR and SSG as most promising carriers. Solid state characteristics of drug-carrier binary system using XRD, DSC techniques revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement in dissolution rate.


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